# US 10,307,428 B2 · Therapeutic compositions for diabetic symmetrical polyneuropathy

> Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt

- Number: US 10,307,428 B2
- Document ID: US10307428B2
- Status: Granted
- Kind: B2
- Application number: 13/877,619
- Filed: 2011-10-24
- Published: 2013-10-10
- Granted: 2019-06-04
- Earliest claimed: 2010-10-25
- Assignees: University Health Network; University of Manitoba; The Regents of the University of California
- Applicants: Paul Fernyhough; Nigel A. Calcutt; Lakshmi Kotra
- Inventors: Paul Fernyhough; Nigel A. Calcutt; Lakshmi Kotra
- Web page: https://patentgrep.com/patent/US10307428B2

## CPC

- A61K 31/5513: 1,4-Benzodiazepines, e.g. diazepam {or clozapine}
- A61K 31/46: 8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
- A61K 31/496: Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
- A61K 31/5517: condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
- A61P 25/02: for peripheral neuropathies
- C07D 417/12: linked by a chain containing hetero atoms as chain links
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)

## Abstract

Compositions for therapy of a diabetic symmetrical polyneuropathy a subject in need thereof, the compositions comprising: an effective amount of a muscarinic acetylcholine receptor antagonist exemplified by pirenzepine, telenzepine, atropine, or derivatives thereof or salts thereof or analogs thereof or derivatives thereof, and a pharmacologically acceptable carrier. The composition may be injectable or alternatively, may be applied topically or alternatively, may be delivered orally. A suitable topical composition may comprise a lotion, a cream, a gel, or a viscous fluid. The muscarinic acetylcholine receptor antagonist may be a muscarinic acetylcholine receptor antagonist salt or a muscarinic acetylcholine receptor antagonist derivative or a muscarinic acetylcholine receptor antagonist analog.

## Claims

### Claim 1

A topical composition for use in therapy of diabetic symmetrical polyneuropathy in a subject in need thereof, the composition comprising:
an effective amount of pirenzepine; and
a pharmacologically acceptable carrier comprising an effective amount of a skin penetration enhancer, wherein the effective amount is at least 0.1% by weight of the composition, and wherein the topical composition comprises 10% wt/vol or less of pirenzepine.

### Claim 2 (depends on 1)

The composition according to claim 1, wherein the pharmacologically acceptable carrier additionally comprises one of a thickening agent, an emollient, an antioxidant, an antimicrobial preservative, an emulsifying agent, a water miscible solvent, an alcohol.

### Claim 3 (depends on 1)

The composition according to claim 1, wherein the composition is one of a lotion, a cream, a gel, and a viscous fluid.

### Claim 4 (depends on 1)

The composition according to claim 1, wherein the effective amount of the skin penetration enhancer is at least 0.5% by weight of the composition.

### Claim 5

A topical composition for treatment of diabetic symmetrical polyneuropathy, comprising:
an effective amount of pirenzepine; and
a pharmacologically acceptable topical carrier comprising a non-cationic skin penetration enhancer, and wherein the topical composition comprises 10% wt/vol or less of pirenzepine.

### Claim 6 (depends on 5)

The topical composition according to claim 5, wherein the pharmacologically acceptable topical carrier comprises one or more of a thickening agent, an emollient, an antioxidant, an antimicrobial preservative, an emulsifying agent, a water miscible solvent and an alcohol.

### Claim 7 (depends on 5)

The topical composition of claim 5, wherein the non-cationic skin penetration enhancer is a transdermal skin penetration enhancer.

### Claim 8 (depends on 5)

The topical composition of claim 5, wherein the non-cationic skin penetration enhancer comprises a sulfoxide, an alkanone or a linear fatty acid.

### Claim 9 (depends on 8)

The topical composition of claim 8, wherein the linear fatty acid is a linoleic acid.